Chitosan-based hepatic-targeted nano-particle drug delivery system and preparation method thereof

A drug delivery system and nanoparticle technology, which is applied in the field of chitosan-based liver-targeted nanoparticle drug delivery system and its preparation, can solve the problems of high efficiency, a large amount of materials and drug waste, operation parallelism, and low ball formation rate. Achieve good biocompatibility, reduce drug dosage and administration times, and improve drug efficacy

Inactive Publication Date: 2010-02-10
NANKAI UNIV
View PDF4 Cites 20 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Previous work such as patents CN 1743008A and CN 101254308A mainly prepared glycyrrhetinic acid-modified targeted drug delivery system by ion cross-linking method. Although the ion cross-linking method is simple, the ball forming rate is low, which easily leads to a waste of a large amount of materials and drugs And the operation parallelism needs to be improved; at the same time, the chitosan-based nanoparticles prepared by the ion cross-linking method are electropositive, and are easy to adsorb protein substances and cause precipitation

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Chitosan-based hepatic-targeted nano-particle drug delivery system and preparation method thereof
  • Chitosan-based hepatic-targeted nano-particle drug delivery system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Embodiment 1: Preparation of glycyrrhetinic acid-sulfate chitosan loaded doxorubicin nanoparticles

[0021] 1) Preparation of succinate glycyrrhetinic acid

[0022] Dissolve 10.0mmol of glycyrrhetinic acid and 40.0mmol of succinic anhydride in 100.0mL of pyridine, heat and reflux for 16 hours, concentrate the reaction solution under reduced pressure and then precipitate with water, adjust the pH to 3~4, filter, and recrystallize the solid with methanol aqueous solution , Vacuum drying, the resulting solid is succinate glycyrrhetinic acid.

[0023] 2) Preparation of glycyrrhetinic acid grafted sulfate chitosan

[0024] Dissolve 2.25g, 10.0mmol sulfate chitosan, molecular weight 50000, deacetylation degree 95%, sulfonation degree 0.8, in 112.5mL water and N,N-dimethylformamide mixed solution, water and N, The volume ratio of N-dimethylformamide is 1:10, the concentration of chitosan sulfate is 20.0mg / mL, add 20.0mmol succinate glycyrrhetinic acid, stir until the solutio...

Embodiment 2

[0029] Example 2: Preparation of Glycyrrhetinic Acid-Carboxymethyl Chitosan-loaded Paclitaxel Nanoparticles

[0030] 1) Preparation of glycyrrhetinic acid succinate: the same as in Example 1.

[0031] 2) Preparation of Glycyrrhetinic Acid Grafted Carboxymethyl Chitosan

[0032] 0.44g, 2.0mmol carboxymethyl chitosan, molecular weight 3000, deacetylation degree 90%, carboxylation degree 1.0, was dissolved in the mixed solution of 88.0mL water and N, N-dimethylformamide, water and N , the volume ratio of N-dimethylformamide is 1:1, the concentration of carboxymethyl chitosan is 5.0mg / mL, add 0.2mmol succinate glycyrrhetinic acid, stir until the solution is transparent, add 0.6mmol 1-(3-Dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and 0.6mmol N-hydroxysuccinimide were reacted at 25°C for 24 hours, acetone precipitated, the solid was dissolved in water, and the pH= 7-8, dialyze against water for 3 days, freeze-dry to obtain glycyrrhetinic acid-carboxymethyl chitosan, an...

Embodiment 3

[0035] Embodiment 3: Preparation of glycyrrhetinic acid-sulfate chitosan-loaded hydroxycamptothecin nanoparticles

[0036] 1) Preparation of glycyrrhetinic acid succinate: the same as in Example 1.

[0037] 2) Preparation of glycyrrhetinic acid grafted sulfate chitosan

[0038] 2.41g, 10.0mmol sulfate chitosan, molecular weight 200000, deacetylation degree 75%, sulfonation degree 1.0, was dissolved in 240.0mL water and N, N-dimethylformamide mixed solution, water and N, The volume ratio of N-dimethylformamide is 1:5, the concentration of chitosan sulfate is 10.0mg / mL, add 6.0mmol succinate glycyrrhetinic acid, stir until the solution is transparent, add 9.0mmol 1- (3-Dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and 9.0mmol N-hydroxysuccinimide, reacted at 55°C for 48 hours, precipitated with acetone, dissolved the solid in water, adjusted pH=7~ 8. Dialyze against water for 3 days, freeze-dry to obtain glycyrrhetinic acid-sulfate chitosan, and the substitution degre...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

PropertyMeasurementUnit
particle diameteraaaaaaaaaa
concentrationaaaaaaaaaa
Degree of sulfonationaaaaaaaaaa
Login to view more

Abstract

The invention relates to a chitosan-based hepatic-targeted nano-particle drug delivery system which takes a derivative of glycyrrhetinic acid-modified chitosan as a carrier material and is prepared byembedding an anti-cancer drug, the particle size of nano-particles is 50nm-300nm, and the drug-loading rate is 5-40%; and the carrier material is glycyrrhetinic acid-sulfate chitosan or glycyrrhetinic acid-carboxymethyl chitosan, and the embedded anti-cancer drug is doxorubicin, paclitaxel or hydroxycamptothecin. The chitosan-based hepatic-targeted nano-particle drug delivery system has the beneficial effects that the chitosan and the derivative thereof are non-toxic and have good biocompatibility and anti-tumor effect, the hepatic targeting tendency of glycyrrhetinic acid and excellent biological performance of the chitosan derivative are combined and a novel hepatic-targeted drug delivery system,is developed and prepared; and the hepatic-targeted nano-particle drug delivery system has drug sustained-release function and hepatic targeting property and can reduce the using amount of the drug and the administration times, reduce the toxicity or the side effects of the drug and improvethe efficacy by being used in the treatment of liver diseases, thereby having good application prospects.

Description

technical field [0001] The invention belongs to the field of biomedical materials, and in particular relates to a chitosan-based liver-targeted nanoparticle drug delivery system and a preparation method thereof. Background technique [0002] Malignant tumor is a common and frequently-occurring disease that seriously threatens human health. At present, there is no effective prevention and control measure. According to the United Nations website, the main types of cancers that cause death are: lung cancer, stomach cancer, liver cancer, colon cancer and so on. In 2007, the number of deaths due to liver cancer was as high as 653,000. At present, the main method of clinical treatment of cancer is chemotherapy, but the antitumor drugs used in chemotherapy have serious toxic and side effects on normal organs of the human body. The targeted drug delivery system delivers the drug directly to the lesion site through the carrier material to exert its curative effect. It has the advan...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/36A61K47/28A61K45/00A61K31/704A61K31/337A61K31/4745A61P35/00A61P1/16
Inventor 袁直王蔚田秦王秀华黄微张闯年
Owner NANKAI UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap